Literature summary for 6.1.1.6 extracted from

Farrera-Sinfreu, J.; Espanol, Y.; Geslain, R.; Guitart, T.; Albericio, F.; Ribas de Pouplana, L.; Royo, M.
Solid-phase combinatorial synthesis of a lysyl-tRNA synthetase (LysRS) inhibitory library (2008), J. Comb. Chem., 10, 391-400.

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Cloned(Commentary)

Cloned (Comment)	Organism
expressed in Novablue Escherichia coli cells	Trypanosoma brucei

Inhibitors

Inhibitors	Comment	Organism	Structure
(3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate	strong inhibitory effect	Trypanosoma brucei
(4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide	strong inhibitory effect	Trypanosoma brucei
(4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide	strong inhibitory effect	Trypanosoma brucei
additional information	the solid-phase combinatorial synthesis of a new library with potential inhibitory activity against the cytoplasmic lysyl-tRNA synthetase (LysRS) isoform of Trypanosoma brucei is described. Among the 65 compounds tested, there are 15 that have a mild inhibitory effect at 100 microM, and 3 have a strong effect	Trypanosoma brucei

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
cytoplasm	-	Trypanosoma brucei	5737	-

Organism

Organism	UniProt	Comment	Textmining
Trypanosoma brucei	Q580G3	-	-

Purification (Commentary)

Purification (Comment)	Organism
nickel affinity column. All the products are purified in a Waters semipreparative HPLC system	Trypanosoma brucei

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
ATP + L-lysine + tRNALys	-	Trypanosoma brucei	AMP + diphosphate + L-lysyl-tRNALys	-	?

Synonyms

Synonyms	Comment	Organism
LysRS	-	Trypanosoma brucei
Lysyl-tRNA synthetase	-	Trypanosoma brucei

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.00995	-	(4S)-1-(3-bromo-4-hydroxybenzyl)-4-[hydroxy(L-lysyl)amino]-L-prolinamide	-	Trypanosoma brucei
0.02761	-	(3R,5S)-1-[(6-amino-9H-purin-9-yl)acetyl]-5-carbamoylpyrrolidin-3-yl L-lysylsulfamate	-	Trypanosoma brucei
0.03442	-	(4R)-1-[(3-chloro-4-hydroxyphenyl)acetyl]-4-[(L-lysylsulfamoyl)oxy]-L-prolinamide	-	Trypanosoma brucei

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Release 2023.1 (January 2023)